Global Patent Index - EP 1401822 A1

EP 1401822 A1 20040331 - NAPHTHYL BENZOFURAN DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1)

Title (en)

NAPHTHYL BENZOFURAN DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1)

Title (de)

NAPHTHYL BENZOFURAN DERIVATE ALS PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) INHIBITOREN

Title (fr)

DERIVES DU NAPHTHYL BENZOFURANE INHIBITEURS DE L'INHIBITEUR 1 DE L'ACTIVATEUR DU PLASMINOGENE (PAI-1)

Publication

EP 1401822 A1 20040331 (EN)

Application

EP 02747904 A 20020618

Priority

  • US 0219231 W 20020618
  • US 29970201 P 20010620

Abstract (en)

[origin: WO03000671A1] This invention provides compounds which act as inhibitors of plasminogen activator inhibitor-1 (PAI-1) of the formula (1), wherein: R, R>1<, R>2<, and R>3< are H, alkyl, cycloalkyl, -CH>2<-(cycloalkyl), alkanoyl, halo, hydroxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, perfluoroalkyl, alkoxy, amino, -NH(alkyl), -N(alkyl)>2<, or perfluoroalkoxy; R>4< is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl, aryl, -CH>2<R>5<, -CH(OH)R>5<, -C(O)R>5<, -CH(SH)R>5<, or -G(S)R>5<; R>5< is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl; R>6< is H, alkyl, cycloalkyl, -CH>2<-cycloalkyl, alkylaryl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is an integer of 0-6; A is COOH, or an acid mimic; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds to treat or prevent conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis, and processes for the preparation of such compounds.

IPC 1-7

C07D 307/79; C07D 405/12; A61K 31/34

IPC 8 full level

A61K 31/343 (2006.01); A61K 31/41 (2006.01); A61P 1/04 (2006.01); A61P 3/04 (2006.01); A61P 3/10 (2006.01); A61P 5/00 (2006.01); A61P 7/00 (2006.01); A61P 7/02 (2006.01); A61P 7/04 (2006.01); A61P 9/00 (2006.01); A61P 9/04 (2006.01); A61P 9/06 (2006.01); A61P 9/08 (2006.01); A61P 9/10 (2006.01); A61P 9/12 (2006.01); A61P 11/00 (2006.01); A61P 13/12 (2006.01); A61P 15/00 (2006.01); A61P 17/02 (2006.01); A61P 17/06 (2006.01); A61P 19/08 (2006.01); A61P 19/10 (2006.01); A61P 25/28 (2006.01); A61P 27/02 (2006.01); A61P 35/00 (2006.01); A61P 35/04 (2006.01); A61P 43/00 (2006.01); C07D 307/80 (2006.01); C07D 307/82 (2006.01); C07D 405/12 (2006.01)

CPC (source: EP US)

A61P 1/04 (2017.12 - EP); A61P 3/04 (2017.12 - EP); A61P 3/10 (2017.12 - EP); A61P 5/00 (2017.12 - EP); A61P 7/00 (2017.12 - EP); A61P 7/02 (2017.12 - EP); A61P 7/04 (2017.12 - EP); A61P 9/00 (2017.12 - EP); A61P 9/04 (2017.12 - EP); A61P 9/06 (2017.12 - EP); A61P 9/08 (2017.12 - EP); A61P 9/10 (2017.12 - EP); A61P 9/12 (2017.12 - EP); A61P 11/00 (2017.12 - EP); A61P 13/12 (2017.12 - EP); A61P 15/00 (2017.12 - EP); A61P 17/02 (2017.12 - EP); A61P 17/06 (2017.12 - EP); A61P 19/08 (2017.12 - EP); A61P 19/10 (2017.12 - EP); A61P 25/28 (2017.12 - EP); A61P 27/02 (2017.12 - EP); A61P 35/00 (2017.12 - EP); A61P 35/04 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07D 307/80 (2013.01 - EP US); C07D 405/12 (2013.01 - EP US)

Citation (search report)

See references of WO 03000671A1

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

DOCDB simple family (publication)

WO 03000671 A1 20030103; AR 036100 A1 20040811; BR 0210532 A 20040622; CA 2449844 A1 20030103; CN 1308320 C 20070404; CN 1543456 A 20041103; EP 1401822 A1 20040331; JP 2004534824 A 20041118; JP 4476624 B2 20100609; MX PA03011400 A 20040405; TW I240723 B 20051001; US 2003018067 A1 20030123; US 6599925 B2 20030729

DOCDB simple family (application)

US 0219231 W 20020618; AR P020102314 A 20020620; BR 0210532 A 20020618; CA 2449844 A 20020618; CN 02816187 A 20020618; EP 02747904 A 20020618; JP 2003507076 A 20020618; MX PA03011400 A 20020618; TW 91112529 A 20020610; US 17416602 A 20020618